The present invention is directed to methods and compositions for promoting the activity of the hair follicles of a living organism and, in particular, to compositions, medicaments, and methods for the treatment of the hair follicles of a human scalp to promote the growth of hair thereon.
At birth, the average human scalp has approximately 100,000-150,000 hair follicles. Initially, hair follicles normally exhibit fine lanugo hair shafts, which are commonly referred to as xe2x80x9cbaby hairxe2x80x9d. This lanugo hair xe2x80x9cmaturesxe2x80x9d eventually, into terminal hair shafts, which is the hair most often exhibited during adolescence and adulthood. Thereafter, this terminal hair may remain as such, or it may develop into non-terminal vellus hair, which is commonly referred to as a xe2x80x9cthinningxe2x80x9d of the hair and, in more advanced stages, baldness.
The precise mechanism that triggers the development of non-terminal vellus hair is not precisely understood or agreed upon. However, there have been numerous attempts to provide an effective safe prophylaxis to arrest development of non-terminal vellus hairs and even to stimulate the regeneration of these vellus hairs into terminal hair shafts. Unfortunately, none of these attempts have proven to be fully satisfactory.
Thus, it can be seen that there remains a need for compositions, medicaments, and methods for administering the same, which are effective in stimulating the development of terminal hairs from non-terminal vellus hairs, are safe for use with a human host, and which are easy to administer.
A patient""s hair loss may be attributable to certain underlying symptomatic conditions or drug exposure, such as telogen effluvium and anagen effluvium. The compositions and methods of the invention may be employed to supplement or augment known treatments for such conditions.
To determine specific known causes of hair loss, a history is taken, and a physical examination is conducted. Once a known cause of hair loss is diagnosed for which a known treatment is accepted, then the known treatment can be instituted.
However, even with types of hair loss whose cause is determined and whose treatment is known, the rate of return of the lost hair may often be undesirably slow. It would be desirable, therefore, to be able to treat the patient being treated for a known cause of hair loss to accelerate the return of hair to such patients.
As further background, it is noted that some vasodilators have been tried topically to treat hair loss, and these vasodilators have not been effective. For example, diazoxide has been tried topically on the scalp to promote hair growth, but this was not deemed to be effective.
It would be desirable to provide effective topical treatments of the hair loss conditions for which satisfactory topical treatments are not currently available.
A number of patents and publications have been uncovered which may be relevant to the scalp treatment methods and compositions of the invention set forth herein below. These patents and publications are as follows, in approximate chronological order:
1. U.S. Pat. No. 4,139,619 of Chidsey (1979)
2. U.S. Pat. No. 4,329,338 of Szego et al (1982)
3. U.S. Pat. No. 4,596,812 of Chidsey et al (1986)
4. U.K. Patent Application No. 2 177 919A of Salim (1987)
More specifically, with respect to literature references, the following summaries of their disclosures are provided.
1. French patent no. 336,814 of Ascoli (1904) appears to disclose a composition used to promote hair growth. The composition appears to disclose the active ingredient to be the chlorhydrate of cocaine. The carrier appears to be a grease, such as vaseline, to form a pomade.
2. New York State Journal of Medicine, Vol. 49, (1949), pages 1317-1318, discloses a solution of niacin and procaine hydrochloride that is used for intravenous administration to treat a number of conditions listed in Table 1. The conditions listed include traumatic, degenerative, inflammatory, and miscellaneous conditions, none of which include hair loss. The composition was administered in an isotonic saline solution. There is a disclosure that niacin or nicotinic acid has a vasodilating effect, especially upon the capillary bed.
3. Aslan A, in Med. Klin.: 52, 758, 1759, 1760 (1957), appears to disclose, as indicated in the translation of the Scholzel article referred to below, that procaine has been used in injection or intravenous therapy of old people resulting to better mental and physical performance abilities, increase in muscle strength, improvement of rigidity, and stimulation of hair growth in many cases of baldness.
4. Scholzel, P., in Med. Klin.: 53, 2239 (1958), in an English translation of the article in German, discloses the general content of the Aslan article mentioned above and goes on to disclose findings relating to a specific patient who, after 40 years of alopecia, showed hair growth after intravenous procaine therapy. There is also a disclosure that a person named Kohler, reported in 1957, the use of a combination of procaine with various vitamins in an apparently injectable composition (xe2x80x9cGerioptil pro injectionexe2x80x9d). However, the specific use of effects of the Kohler compositions were not disclosed.
5. French patent no. 1439833 of Serviere (1966) appears to disclose a composition which contains a synergistic combination of the following ingredients: malic acid, procaine, and a soluble derivative of sulfapyridine. The composition is apparently applied topically to improve hair characteristics, but not necessarily hair growth.
6. U.S. Pat. No. 3,644,364 of Anthony (1972) discloses a process for preparing compounds which include minoxidil, an agent that may promote hair growth.
7. Chemical Abstracts No. 79:23508s (1973) discloses an abstract of a German patent (to Indal Oy) that discloses hair growth promoting characteristics. The disclosures in the German patent of Indal Oy appear to be similar to the disclosures in French patent no. 72.39675 of Indal Oy (1973) and UK patent no. 1 354 446 of Indal Oy (1974) mentioned below.
8. French patent no. 72.39675 of Indal Oy (1973) appears to disclose the compositions that are disclosed in UK patent no. 1 354 446 of Indal Oy (1974).
9. UK Patent No. 1 354 446 of Indal Oy (1974) discloses a composition for promoting the growth of hair. The composition contains nicotinic acid and salicylic and/or benzoic acid dissolved in a carrier containing ethanol, urea, polyoxyethylene sorbitan-monopalmitate or monostearate, with the remainder being isopropyl myristate.
10. U.S. Pat. No. 3,952,099 of Smith (1976) is very similar in its disclosure to U.S. Pat. No. 3,896,238 to Smith (1975).
11. U.S. Pat. No. 4,139,619 of Chidsey (1979) discloses compositions which employ minoxidil in carriers to be applied topically to a scalp to promote hair growth.
12. UK Patent No. 1 603 639 of Haggar (1981) discloses a composition for application to the hair and scalp for use in stimulating hair growth in treating alopecia and excessive hair loss. The composition includes a hair conditioner (lotion or cream) and a vitamin solution which contains vitamins B1, B2, B2, A, D, nicotinamide, and ascorbic acid. It has been found particularly advantageous to use Oil of Rosemary in the vitamin solution. More specifically, in one preferred embodiment, Oil of Rosemary is included. In another preferred embodiment, Oil of Balsam is included. In addition, the carrier can be the conditioner LIFE-TEX (T.M.) produced by Wella, which has been found satisfactory. The carrier desirably promotes absorption into the scalp and is preferably an antiseptic type spirit which may be alcohol, isophane insulin, or other biologically acceptable volatile liquid. However, white iodine is the preferred carrier. Petroleum jelly or liquid paraffin may also be included. There is a statement that the composition for application to the hair and scalp includes a commercial hair conditioner and a vitamin solution which contains one or more of the disclosed vitamins.
13. U.S. Pat. No. 4,329,338 of Szego et al (1982) discloses compositions for use as cosmetics. The compositions include a reaction product of nicotinic acid, a nicotinic acid salt, or a nicotinic acid halide and a polyhyroxy compound whose general formula is given in the Abstract. The active agents are disclosed as exerting beneficial effects for stimulating scalp or hair bulbs.
14. U.S. Pat. No. 4,596,812 of Chidsey et al (1986) discloses methods and compositions for treating male pattern alopecia. The compositions include the substance known as minoxidil. Minoxidil is disclosed as a vasodilator that functions to dilate the peripheral vascular system. Minoxidil compositions are applied topically to the scalp and are used in a carrier system which can include equal parts of ethyl alcohol and propylene glycol.
15. UK patent application on. 2 176 104A of Grollier (1986) discloses compositions for the treatment of hair and of the scalp to promote fresh hair growth. It is disclosed that compositions containing nicotinic acid or its esters, when applied to the scalp, have rubefacient and vasodilant activity. The specific compositions disclosed in this patent include the combination of certain water-soluble polyamides of the poly-beta-alanine type with nicotinic acid or its esters. As shown in Examples 1 and 4, for a hair-care lotion, the carrier includes ethyl alcohol and water.
16. UK patent application on. 2 177 919A of Salim (1987) discloses, in Example 9, a topical preparation to restore hair growth to areas of the human scalp suffering from hair loss. The preparation includes procaine, a physiologically acceptable, organic, in vivo sulphydryl group releasing agent, and castor oil.
The following conclusions can be made from a consideration of the prior art discussed above. Procaine has been used topically, in the presence of other active ingredients and in the presence of complex carrier ingredients, often including sulfur-containing carriers, to treat the scalp for hair growth. It is also clear from the prior art that neither procaine nor niacin, either alone or in combination with one another, has been used topically without other active ingredients and without a complex carrier system which often includes sulfur-containing carriers and non-hydrophilic ingredients.
Carriers containing sulfur-containing ingredients have their problems. for example, the safety and efficacy of dimethylsulfoxide (DMSO) has not been sufficiently established for the U.S. Food and Drug Administration to permit its use in the United States.
Carriers containing non-hydrophilic ingredients may have the undesirable property of impeding or preventing penetration of the active, hair-bulb treating agents into the hair bulb from the surface of the skin when the active ingredient is applied topically.
Accordingly, it is a primary object of the present invention to alleviate the disadvantages and deficiencies of the prior at by providing compositions and medicaments that are effective for stimulating the development (growth) of terminal hairs from the hair bulb of non-terminal vellus hair follicles.
It is another primary object of the present invention to provide compositions and medicaments which may safely be used with a human host.
It is still another primary object of the present invention to provide methods for stimulating the development (growth) of terminal hairs from the hair bulb of non-terminal vellus hair follicles.
Another object of the present invention is to provide topical methods of treating scalp hair loss and to stimulate scalp hair growth by employing solutions containing simply procaine (or a derivative thereof) and/or niacin in a simple, water-miscible carrier.
Still another object of the invention is to provide a topically applied composition that includes an agent that will stimulate hair growth by stimulating the hair bulb and that also includes a non-sulfur-containing carrier.
Yet another object of the invention is to provide a topically applied composition that includes an agent that will stimulate hair growth by stimulating the hair bulb and that also contains a carrier that does not include a sulfur-containing ingredient.
Still another object of the invention is to provide a topically applied composition that includes an agent for stimulating hair growth by stimulating the hair bulb and that also contains a carrier that does not contain non-hydrophilic ingredients.
In accordance with the teachings of the present invention, there is disclosed the use of a secondary or tertiary amino local anesthetic for the manufacture of a topical medicament for stimulating the growth of a hair bulb of a vellus hair follicle.
Preferably, the secondary or tertiary amino local anesthetic is either a secondary or tertiary amino ester of para-aminobenzoic acid, or a secondary or tertiary amino type ester of either benzoic acid or meta-aminobenzoic acid, or a secondary or tertiary amino type amide or a secondary or tertiary amino type ether, or a secondary or tertiary amino type ketone.
In further accordance with the teachings of the present invention, there is disclosed the use of niacin for the manufacture of a topical medicament for stimulating the growth of a hair bulb of a vellus hair follicle.
In yet another aspect of the present invention, methods are disclosed for stimulating the growth of a hair bulb for a vellus hair follicle that involves the topical administration of a therapeutic amount of the medicaments described above to a patient in need thereof.
In still further accordance with the teachings of the present invention, a composition for stimulating the growth of a hair bulb of a vellus hair follicle is disclosed. This composition includes either a secondary or tertiary amino local anesthetic or niacin as its active ingredient. This composition further includes a pharmaceutically-acceptable carrier.
Preferably, the carrier is a hydrophilic carrier that does not have a sulfur-based ingredient and that may be chosen from the group consisting of propylene glycol, absolute alcohol, and isopropyl alcohol. Alternatively, a combination of two or more of these carriers may be employed.
In another aspect of the present invention, there is disclosed a method for stimulating the growth of a hair bulb of a vellus hair follicle. This method includes, first, preparing a composition for stimulating the growth of a hair bulb of a vellus hair follicle which includes either niacin or a secondary or tertiary amino local anesthetic as its active ingredient, and a hydrophilic carrier; and second, topically applying the composition to a scalp having a vellus hair follicle in need thereof